Dimethylformamide → 4-[7-(3-Imidazol-1-ylprop-1-ynyl)-1-oxo-1H-5-azaisoquinolin-2-ylmethyl]benzoic Acid tert-Butyl Ester

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Reaction Steps

The coupling of 4-(7-bromo-1-oxo-1H-5-azaisoquinolin-2-ylmethyl)benzoic acid tert-butyl ester (0.80 g, 1.93 mmol) with 4-prop-2-ynyl-4H-triazole (0.41 g, 3.86 mmol) using triethylamine (1.08 mL, 7.22 mmol), CuI (0.026 g, 0.14 mmol), and Pd(Ph3P)4 (0.15 g, 0.13 mmol) in dimethyl-formamide is carried out as described in Example 1, Step (2). Purification on a silica gel column eluted with hexane/ethyl acetate 2:1, ethyl acetate, and methylene chloride/THF 4:1, followed by drying, will afford the desired product.

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